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Synthesis and Preliminary Pharmacological Evaluation of Aminobenzensulfonamides Derivatives of Mefenamic Acid as a Potential Anti-inflammatory Agents
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A group of amino derivatives [4-aminobenzenesulfonamide,4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent.  In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-amino-N-methylbenzenesulfonamide derivative (compound 10) exhibited comparable anti-inflammatory activity to diclofenac (3mg/Kg) at times 180-300 minute with the same onset of action. The results of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore and its derivatives in to mefenamic acid maintain its anti-inflammatory activity.

Key ward: benzenesulfonamide, anti-inflammatory, paw edema, NSAIDs, mefenamic   acid

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Publication Date
Sun Mar 08 2020
Journal Name
Biochem. Cell. Arch
SYNTHESIS AND SPECTROSCOPIC CHARACTERIZATION OF NEW HETEROCYCLIC COMPOUNDS DERIVATIED FROM 1-(4-AMINOPHENYL) ETHAN-1-ONEOXIME AS A STARTING MATERIAL WITH EVALUATE THEIR BIOLOGICAL ACTIVITY
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ABSTRACT : This research involves the synthesis of five to seven heterocyclic compounds starting with Schiff’s bases which derived from oxime as a starting material. 1.3-oxazepine derivatives were prepared from adding different anhydrides to the Schiff bases, tetrazole and thiazolidinone derivatives synthesized from add sodium azide and thioglycolic acid to the same Schiff’s bases as a five members ring. Pyrimidine derivatives were prepared after the reaction of the azomethine group with acetyl chloride and then urea and thiourea to synthesis on derivatives contain the six members ring. Another step included identified and confirmed these compounds by FT- IR, 1HNMR, TLC and 13CNMR finally, step included the assay of biological activity

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Publication Date
Wed May 01 2013
Journal Name
Chemical And Process Engineering Research
Synthesis and Characterization of Polycyclicacetal Derived from PEG & Erythro-Ascorbic Acid Derivative and Study Its Effect on the Activity of ACh Enzyme (In Vitro)
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Polycyclicacetal was prepared from the reaction of PEG with aldehyde derived from Erythro-ascorbic acid (pentulosono-ɣ-lactone-2,3-enedianisoate).All these compounds were characterized by Thin Layer Chromatography (TLC) and FTIR spectra and aldehyde was also characterized by (U.V-Vis), 1HNMR, 13CNMR, and mass spectra.The inhibitory effect of prepared polymer on the activity of human serum AcetylCholinesterase has been studied in vitro. The polymer showed a remarkable activity at low concentration (4.7x10-3 – 4.7x10-8M).

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Publication Date
Mon Aug 29 2022
Journal Name
Indonesian Journal Of Chemistry
Synthesis, DFT Calculations, DNA Interaction, and Antimicrobial Studies of Some Mixed Ligand Complexes of Oxalic Acid and Schiff Base Trimethoprim with Various Metal Ions
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Mixed ligand metal complexes are synthesized from oxalic acid with Schiff base, and the Schiff base was obtained from trimethoprim and acetylacetone. The synthesized complexes were of the type [M(L1)(L2)], where the metal, M, is Ni(II), Cu(II), Cr(III), and Zn(II), L1 corresponds to the trimethoprim ((Z)-4-((4-amino-5-(3,4,5-trimethoxybenzyl)pyrimidine-2-yl)imino)pentane-2-one) as the first ligand and L2 represent the oxalate anion ( ) as a second ligand. Characterization of the prepared compounds was performed by elemental analysis, molar conductivity, magnetic measurements, 1H-NMR, 13C-NMR, FT-IR, and Ultraviolet-visible (UV-Vis) spectral studies. The recorded infrared data is reinforced with density functional theory (DFT) calcul

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Publication Date
Sat Jul 01 2023
Journal Name
Indones. J. Ch Em
Synthesis, DFT Calculations, DNA Interaction, and Antimicrobial Studies of Some Mixed Ligand Complexes of Oxalic Acid and Schiff Base Trimethoprim with Various Metal Ions
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Mixed ligand metal complexes are synthesized from oxalic acid with Schiff base, and the Schiff base was obtained from trimethoprim and acetylacetone. The synthesized complexes were of the type [M(L1)(L2)], where the metal, M, is Ni(II), Cu(II), Cr(III), and Zn(II), L1 corresponds to the trimethoprim ((Z)-4-((4-amino-5-(3,4,5- trimethoxybenzyl)pyrimidine-2-yl)imino)pentane-2-one) as the first ligand and L2 represent the oxalate anion (𝐶􀬶𝑂􀬶 􀬶􀬿) as a second ligand. Characterization of the prepared compounds was performed by elemental analysis, molar conductivity, magnetic measurements, 1H-NMR, 13C-NMR, FT-IR, and Ultraviolet-visible (UV-Vis) spectral studies. The recorded infrared data is reinforced with density functional th

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Publication Date
Thu Aug 15 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis, Characterization and Study of the Biological Activity of New Metal Complexes of Ligand[2-(3-benzoylthioureido)-3-(-4- hydroxyphenyl) Propanoic Acid (BHP)
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In this paper, series of new complexes of Manganese(II), Cobalt(II), Nickel (II) Cupper(II) Zinc(II), Cadmium(II) and Mercury (II) are prepared from the new ligand [2-(3-benzoylthioureido)-3-(-4- hydroxyphenyl) propanoic acid (BHP) derived from tyrosine and benzoylisothiocyanate .Chemical structures are obtained from their 1 H, 13CNMR spectra (for BHP), elemental microanalyses, molar conductance, FTIR, UV–Vis, magnetic susceptibility in addition to TGA/DTG and DSC analysis, the suggested geometry for all complexes was tetrahedral. The biological activity of BHP and its complexes has been extensively studied against two bacterial species Staphylococcus aurous (G+) and Escherichia coli (G-) by agar-well diffusion technique, where Mn(II), Co

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Publication Date
Mon Dec 18 2017
Journal Name
Agronomy
A Case Study of Potential Reasons of Increased Soil Phosphorus Levels in the Northeast United States
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Recent phosphorus (P) pollution in the United States, mainly in Maine, has raised some severe concerns over the use of P fertilizer application rates in agriculture. Phosphorus is the second most limiting nutrient after nitrogen and has damaging impacts on crop yield if found to be deficient. Therefore, farmers tend to apply more P than is required to satisfy any P loss after its application at planting. Several important questions were raised in this study to improve P efficiency and reduce its pollution. The objective of this study was to find potential reasons for P pollution in water bodies despite a decrease in potato acreage. Historically, the potato was found to be responsible for P water contamination due to its high P sensitivity a

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Publication Date
Sat Jan 01 2022
Journal Name
Revista Electronica De Veterinaria
Antibacterial and Anti Biofilm activity of Eucalyptus Plant Extract Spp
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Publication Date
Mon Dec 30 2024
Journal Name
Iraqi Journal Of Science
The Impact of Fear and Anti-Predator Behavior on the Dynamics of Stage-Structure Prey–Predator Model With a Harvesting
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In this paper, an ecological model with stage-structure in prey population, fear, anti-predator and harvesting are suggested. Lotka-Volterra and Holling type II functional responses have been assumed to describe the feeding processes . The local and global stability of steady points of this model are established. Finally, the global dynamics are studied numerically to investigate the influence of the parameters on the solutions of the system, especially the effect of fear and anti-predation.

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Publication Date
Tue Jan 01 2019
Journal Name
Baghdad Science Journal
Synthesis of new five-membered hetrocyclic compounds from 2-furfuryl mercaptan derivative and evaluation of their biological activity
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A theoretical and protection study was conducted of the corrosion behavior of carbon steel surface with different concentrations of the derivative (Quinolin-2-one), namly (1-Amino-4,7-dimethyl-6-nitro-1H-quinolin-2-one (ADNQ2O)). Theoretically, Density Functional Theory (DFT) of B3LYP/ 6-311++G (2d, 2p) level was used to calculate the optimized geometry, physical properties and chemical inhibition parameters, with the local reactivity to predict both the reactive centers and to locate the possible sites of nucleophilic and electrophilic attacks, in vacuum, and in two solvents (DMSO and H2O), all at the equilibrium geometry. Experimentally, the inhibition efficiencies (%IE) in the saline solution (of 3.5%) NaCl were studied using potentiomet

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Publication Date
Fri Jun 28 2024
Journal Name
Al-rafidain Journal Of Medical Sciences ( Issn 2789-3219 )
Synthesis, Characterization, Molecular Docking, ADMET Study, and Antimicrobial Evaluation of New Mannich Bases of Isatin–Thiazole Imine Bases
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Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted o

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